Table 2. Antiviral Potencies in Cells Infected with HIV-1 Vectors That Carry WT or Resistant IN Mutants.
| EC50 (nM)c,d |
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|---|---|---|---|---|---|---|
| no. | CC50 (μM)a | EC50 (nM)b | Y143R | N155H | G140S/Q148H | G118R |
| 1e | > 250 | 4 ± 2 | 162 ± 16 (41) | 154 ± 33 (39) | 1900 ± 300 (475) | 36 ± 5 (9)e |
| 2 | > 250 | 6.4 ± 0.8 | 7.9 ± 2.3 (1.2) | 90 ± 18 (14) | 5700 ± 1100 (891) | 21 ± 10 (3.3) |
| 3e | > 250e | 1.6 ± 0.9e | 4.3 ± 1.2 (2.7)e | 3.6 ± 1.3 (2.3)e | 5.8 ± 0.5 (3.6)e | 13 ± 5 (8.1)e |
| 4ae | > 250e | 1.1 ± 0.7e | 2.5 ± 0.6 (2.3)e | 5.3 ± 2.3 (4.8)e | 35 ± 9 (32)e | 16 ± 5 (15)e |
| 4b | > 250 | 3.1 ± 2.0 | 2.8 ± 0.9 (0.90) | 8.5 ± 3.1 (2.7) | 13.4 ± 6.5 (4.3) | 10 ± 1.6 (3.2) |
| 4c | > 250 | 1.3 ± 0.2 | 3.0 ± 0.5 (2.3) | 2.4 ± 0.8 (1.8) | 6.9 ± 2.3 (5.3) | 5.3 ± 1.6 (4.1) |
| 4d | > 250 | 2.3 ± 0.6 | 2.1 ± 1.4 (0.91) | 2.7 ± 1.0 (1.2) | 9.4 ± 3.6 (4.1) | 6.4 ± 2.5 (2.8) |
| 4e | > 250 | 3.7 ± 0.4 | 3.2 ± 0.8 (0.86) | 6.5 ± 2.7 (1.8) | 7.7 ± 1.9 (2.1) | 11 ± 1 (3.0) |
| 4f | > 250 | 2 ± 0.1 | 0.6 ± 0.1 (0.3) | 2.1 ± 1.2 (1) | 5.2 ± 0.3 (3) | 11.4 ± 3.5 (6) |
| EC50 (nM)c,d |
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|---|---|---|---|---|---|
| no. | R263K | T66I | E92Q | H51Y | H51Y/R263K |
| 1e | 5.7 ± 2.3 (1.4)e | 2.8 ± 0.4 (0.7) | 30 ± 10 (7.5) | 3.4 ± 0.2 (0.2) | 6 ± 2.3 (1.5) |
| 2 | 10 ± 6 (1.6) | 66 ± 1 (10) | 154 ± 34 (24) | 4.5 ± 2.1 (0.7) | 53 ± 18 (8) |
| 3e | 11 ± 3 (6.9)e | 0.9 ± 0.8 (0.56) | 2.3 ± 0.4 (1.4) | 3.2 ± 0.2 (2) | 16 ± 2 (10) |
| 4ae | 6.4 ± 2.3 (5.8)e | 0.6 ± 0.3 (0.54) | 3.0 ± 1.8 (2.7) | 1.0 ± 0.6 (0.91) | 3.2 ± 0.9 (2.9) |
| 4b | 2.5 ± 0.8 (0.81) | 1.1 ± 0.1 (0.35) | 4.8 ± 2.0 (1.5) | 2.6 ± 0.5 (0.84) | 15 ± 2 (4.8) |
| 4c | 2.6 ± 0.1 (2.0) | 0.93 ± 0.24 (0.72) | 3.8 ± 2.3 (2.3) | 3.8 ± 0.6 (2.9) | 2.6 ± 1.4 (2.0) |
| 4d | 8.4 ± 2.3 (3.7) | 0.50 ± 0.35 (0.22) | 0.74 ± 0.13 (0.32) | 1.6 ± 0.1 (0.70) | 5.2 ± 1.6 (2.3) |
| 4e | 3.8 ± 1.1 (1.0) | 1.7 ± 0.5 (0.46) | 2.6 ± 0.2 (0.70) | 4.8 ± 1.1 (1.3) | 22 ± 8 (5.9) |
| 4f | 5.3 ± 0.8 (2) | 0.7 ± 0.1 (0.3) | 1.2 ± 0.6 (0.6) | 0.8 ± 0.5 (0.4) | 5.3 ± 0.4 (2) |
a
Cytotoxic concentration resulting in 50% reduction in the level of ATP in human osteosarcoma (HOS) cells.
b
Values obtained from cells infected with a lentiviral vector carrying WT IN.
c
Cells were infected with viral vectors carrying IN mutations. The table shows the EC50 values.
d
Fold-change (FC) in EC50 relative to WT.
e
Previously reported values.24